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[nat/89Zr][Zr(pypa)]: Thermodynamically Stable and Kinetically Inert Binary Nonadentate Complex for Radiopharmaceutical Applications

Title[nat/89Zr][Zr(pypa)]: Thermodynamically Stable and Kinetically Inert Binary Nonadentate Complex for Radiopharmaceutical Applications
Publication TypeJournal Article
Year of Publication2021
AuthorsSouthcott, L, LI, LILY, Patrick, BO, Stephan, H, Jaraquemada-Pelaez, Mde Guadalu, Orvig, C
JournalInorg. Chem.
Volume60
Pagination18082-18093
Date Published11/2021
Abstract

{ H4pypa is a nonadentate nonmacrocyclic chelator, which previously demonstrated high affinity for scandium-44, lutetium-177, and indium-111. Herein, we report the highly stable binary [Zr(pypa)] complex; the nonradioactive complex was synthesized and characterized in detail using high-resolution electrospray-ionization mass spectroscopy (HR-ESI-MS) and various nuclear magnetic resonance spectroscopies (NMR), which revealed C2v symmetry of the complex. The geometry of [Zr(pypa)] was further detailed via X-ray crystallography and compared with the structure of [Fe(Hpypa)]. Despite a slow complexation rate with an association half-life of 31.4 h at pH 2 and room temperature, the [Zr(pypa)] complex is thermodynamically stable (log KML = 38.92

URLhttps://doi.org/10.1021/acs.inorgchem.1c02709
DOI10.1021/acs.inorgchem.1c02709
Refereed DesignationRefereed